title: Molecular pharmacology of store-operated CRAC channels.
abstract: Calcium influx through store-operated Ca(2+) release-activated Ca(2+) channels (CRAC channels) is a well-defined mechanism of generating cellular Ca(2+) elevations that regulates many functions including gene expression, exocytosis and cell proliferation. The identifications of the ER Ca(2+) sensing proteins, STIM1-2 and the CRAC channel proteins, Orai1-3, have led to improved understanding of the physiological roles and the activation mechanism of CRAC channels. Defects in CRAC channel function are associated with serious human diseases such as immunodeficiency and auto-immunity. In this review, we discuss several pharmacological modulators of CRAC channels, focusing specifically on the molecular mechanism of drug action and their utility in illuminating the mechanism of CRAC channel operation and their physiological roles in different cells.
authors.affiliation: Department of Molecular Pharmacology and Biological Chemistry; Northwestern University, Feinberg School of Medicine; Chicago, IL USA.
authors.forename: Amit
authors.initials: A
authors.lastname: Jairaman
authors.affiliation: Department of Molecular Pharmacology and Biological Chemistry; Northwestern University, Feinberg School of Medicine; Chicago, IL USA.
authors.forename: Murali
authors.initials: M
authors.lastname: Prakriya
mesh_terms: D000818:Animals; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D015220:Calcium Channels / Q000737:chemistry / Q000378:metabolism*; D020013:Calcium Signaling / Q000187:drug effects; D004721:Endoplasmic Reticulum / Q000378:metabolism; D006801:Humans; D008565:Membrane Proteins / Q000737:chemistry / Q000378:metabolism; D009363:Neoplasm Proteins / Q000737:chemistry / Q000378:metabolism; D011487:Protein Conformation; D000071737:Stromal Interaction Molecule 1
chemical_list: D002121:Calcium Channel Blockers; D015220:Calcium Channels; D008565:Membrane Proteins; D009363:Neoplasm Proteins; C103530:STIM1 protein, human; D000071737:Stromal Interaction Molecule 1
keywords: CRAC channel; Orai1; SOCE; STIM1; pharmacology